Good Entrapment Efficiency Research Articles

Oral delivery of solid lipid nanoparticles surface decorated with hyaluronic acid and bovine serum albumin: A novel approach to treat colon cancer through active targeting

The present study aims to prepare and evaluate solid lipid nanoparticles (SLNs) loaded with irinotecan (IRN) drug and daidzein (DZN) isoflavonoid and surface coated with ligand materials such as hyaluronic acid (HA) and bovine serum albumin (BSA) with additional coating of chitosan for active targeting to receptors present on colon surface epithelium for oral targeted delivery. The optimized batch was evaluated for particle size, zeta potential exhibiting nanometric size with good entrapment efficiency. Nanoparticles were found to be spherical. FTIR and DSC revealed that all the excipients and formulation were compatabile to each other and showed better encapsulation exhibiting amorphous and crystallinity forms. In vitro drug release of SLNs confirmed that initially a burst release, followed by sustained release pattern was exhibited. Cell lines studied performed on HT-29 cells showed demonstrated that conjugated SLNs inhibited cytotoxicity at 75 μg/ml, indicating that cells were taken up through a receptor-mediated endocytosis process. Cell cycle analysis showed that cell arrest was done at 67.8 % (G0/G1 phase) and inhibited apoptosis by 56 %. Further during In vivo studies, RT-PCR study revealed downregulation of Carcinoembryonic antigen (CEA), a non-specific serum biomarker overexpressed in tumor cells and upregulation of pro-inflammatory cytokine TNF-α. Histopathological study revealed that conjugated (HA-BSA) coated with chitosan SLNs restored normal mucosa and colon architecture, depicting all mucosal layers. Hence, these conjugated SLNs may serve as a novel combination for the treatment of colon cancer.

Box–Behnken design for the development of fluconazole-loaded classical ethosomes

Introduction: Ethosomes are soft and flexible vesicles mainly composed of phospholipids, ethanol and water. The presence of a high amount of ethanol ensure deeper drug penetration; however, an optimal formulation is necessary. This study aims to develop and characterize Fluconazole loaded classical ethosomes using Box-Behken design, in order to achieve to an optimal formulation having a minimal vesicle size, low polydispersity index, high zeta potential and good entrapment efficiency (% EE). Methods: Fluconazole ethosomes were prepared using cold method and tested for vesicle size, polydispersity index, zeta potential and EE%. Box-Behken design was created using Design Expert® Software, where the impact of sonication time and amount of ethanol and soybean lecithin on resulting formulation were investigated. Results: It was determined that increasing the concentration of ethanol up to an optimized limit reduces vesicle size and improves % EE. It was also observed that soybean lecithin concentrations affected positively vesicle size but negatively % EE. Whereas sonication time had an inverse effect both on, vesicle size and EE%. All prepared formulations showed a low polydispersity index and a good zeta potential indicating homogeneity and high stability. Therefore, the optimal formulation had % EE of 80.05±0.306 % and vesicular size of 226.501±5.34 nm with polydispersity index of 0.487±0.0078. Conclusion: In summary, using Box-Behnken design can enhance the understanding of the correlations between the variables involved in ethosome formation and their effects on vesicle size, polydispersity index and % EE. The optimal formulation obtained can be incorporated into drug delivery systems to enhance skin permeation and antifungal activity.

Modified Release Interpenetrating Polymeric Network Hydrogel Beads of Montelukast Sodium Via Box Behnken Design

Background: Interpenetrating Polymeric Networks (IPN) are cross-linked polymeric alloys developed when two or more cross-linked polymers inter-penetratingly entangle. Interpenetrating polymeric networks possess several benefits including stability, biocompatibility, biodegradability, high swelling ability, and modified release efficiency. Aim: The aim of this study is to design stable, control-released montelukast sodium-loaded IPN hydrogel beads as a promising approach toward drug delivery. Objective: The goal of the present work was to develop Chitosan (swellable polymer) and glutaraldehyde (cross-linker) based modified (controlled) released montelukast sodium IPN hydrogel beads. Methods: The montelukast sodium IPN hydrogel beads were prepared via the precipitation method, and the final batch of IPN hydrogel beads was based on particle size, percent entrapment efficiency, area of swelling, and cumulative percent drug release using an overlay plot in Box-Behnken design. Compatibility studies (DSC, FT-IR) and microscopical observation (SEM) confirmed the compatibility and sphericity of the formulations. Results: The optimized (comprising 2.01% chitosan and 0.48% glutaraldehyde) IPN hydrogel beads having satisfactory particle size (817.76±54.49 μm), good entrapment efficiency (71.36±3.04%), and area of swelling (27.00±1.68 mm2) showed swelling and pH-dependent controlled montelukast release (92.96±1.05%) after 12 h with longer duration of action. Conclusion: The prepared montelukast sodium IPN hydrogel beads could be a potent control-released drug delivery vehicle.

Virgin Coconut Oil-based Nanostructured Lipid Carrier Improves the Hypolipidemic Effect of Rosuvastatin.

Monitoring noncommunicable diseases is regarded as a critical concern that has to be managed in order to avoid a wide variety of complications such as increasing blood lipid levels known as dyslipidemia. Statin drugs, mostly, Rosuvastatin (RSV) was investigated for its effectiveness in treating dyslipidemia. However, reaching the most efficient treatment is essential and improving the effect of RSV is crucial. Therefore, a combination therapy was a good approach for achieving significant benefit. Although RSV is hydrophobic, which would affect its absorption and bioavailability following oral administration, overcoming this obstacle was important. To that end, the purpose of the present investigation was to incorporate RSV into certain lipid-based nanocarriers, namely, nanostructured lipid carrier (NLC) prepared with virgin coconut oil (CCO). The optimized RSV-NLC formula was selected, characterized and examined for its in vitro, kinetic, and stability profiles. Eventually, the formula was investigated for its in vivo hypolipidemic action. The optimized NLC formulation showed a suitable particle size (279.3±5.03 nm) with PDI 0.237 and displayed good entrapment efficiency (75.6±1.9%). Regarding in vitro release, it was efficiently prolonged for 24 h providing 93.7±1.47%. The optimized formula was established to be stable after 3 months storage at two different conditions; 4°C and 25°C. Importantly, including CCO in the development of RSV-NLC could impressively enhance lowering total cholesterol level in obese rat models, which endorse the potential synergistic action between RSV and CCO. The study could elucidate the impact of developing NLC using CCO for improving RSV anti-hyperlipidemic activity.

Formulation and Evaluation of Nanosuspension of Mebendazole for Solubility Enhancement by High Pressure Homogenization Technique

Background: Developing and evaluating a drug taken by mouth delivery method with mebendazole nanosuspension to treat intestinal worms infestations are the main objectives of the current research effort. This is because drug particles in the nano range help to reduce particle size and enhance dissolution. Methods: By using High pressure homogenization method, the mebendazole is converted into nanosuspension. Various amounts of HPMC K4M used as a stabilizer and Tween 80 and Poloxamer 188 used as a surfactant and compare its ratios. The results were investigated using effectiveness of drug entrapment, saturation solubility, zeta potential, particle size, drug release study and stability testing. Result: The drug purification results are shown by knowing the FT-IR spectrum. With a good entrapment efficiency and saturated solubility, optimized batches are found and the use of transmission electron microscopy confirms the nano size particle formed. The mebendazole nanosuspension showed higher release in the target site within 12 hours, according to an in-vitro dissolution experiment. Using the oral route for administration of the mebendazole nanosuspension, it increases the drugs absorption along with complete drug releasing. Conclusion: The study indicates that the prepared mebendazole nanosuspension has increased the rate of dissolution and solubility by converting nano range particles and encouraging the use of BCS class Ⅱ drugs with acceptable stability.

A promising eco-sustainable wound dressing based on cellulose extracted from Spartium junceum L. and impregnated with Glycyrrhiza glabra L extract: Design, production and biological properties

Glycyrrhiza glabra extract is widely known for its antioxidant and anti-inflammatory properties and can improve the wound healing process. The aim of this work was to shorten the time of the healing process by using an eco-sustainable wound dressing based on Spanish broom flexible cellulosic fabric by impregnation with G. glabra extract-loaded ethosomes. Chemical analysis of G. glabra extract was performed by LC-DAD-MS/MS and its encapsulation into ethosomes was obtained using the ethanol injection method. Lipid vesicles were characterized in terms of size, polydispersity index, entrapment efficiency, zeta potential, and stability. In vitro release studies, biocompatibility, and scratch test on 3T3 fibroblasts were performed. Moreover, the structure of Spanish broom dressing and its ability to absorb wound exudate was characterized by Synchrotron X-ray phase contrast microtomography (SR-PCmicroCT). Ethosomes showed a good entrapment efficiency, nanometric size, good stability over time and a slow release of polyphenols compared to the free extract, and were not cytotoxic. Lastly, the results revealed that Spanish broom wound dressing loaded with G. glabra ethosomes is able to accelerate wound closure by reducing wound healing time. To sum up, Spanish broom wound dressing could be a potential new green tool for biomedical applications.

An Overview of Transferosomal Technology

Abstract: Ever since the invention of liposomes by Bangham in 1963, researchers have been fascinated by the vesicular carriers. Liposomes and niosomes have been used extensively by researchers for various routes such as oral and nasal. However, lately, it has been understood that traditional liposomes are not very significant when it comes to penetration. The use of nanovesicles in transdermal drug delivery systems has been enhanced exponentially ever since the discovery of ultra- deformable liposomes known as transfersomes or transferosomes. Transferosomes have numerous advantages, such as biocompatibility, biodegradability, flexibility, and deformability, so that they can pass through narrow constrictions. They have good entrapment efficiency and can act as a depot to sustain the release of drugs. The methods of preparation include the rotary film evaporation method, reverse phase evaporation method, vortexing sonication method, ethanol injection method, and freeze-thaw method. Transfersomes are characterized by particle size, zeta potential, polydispersity index, surface morphology, and encapsulation efficiency. Transferosomes have been successfully exploited for the enhancement of efficacy of many drugs like Hydroquinone, Itraconazole, Ivabradine, lornoxicam, minoxidil etc., via transdermal and nasal routes. The technology is easy to scale up. Consequently, it can be inferred that transfersomes are the future of transdermal drug delivery systems.

In vitro cytotoxic and genotoxic effects of Phyllanthus niruri extract loaded chitosan nanoparticles in TM4 cells and their influence on spermatogenesis

Purpose: This paper introduces a complete in vitro investigation of cytotoxic and genotoxic effects of Phyllanthus niruri extract loaded chitosan nanoparticles (PNNP) on mouse Sertoli cell line (TM4), as well as their impact on spermatogenesis. Methods: Chitosan nanoparticles (ChNP) and PNNP were prepared using an ionic gelation process, while their cytotoxicity on TM4 cells was assessed using the Cell Counting Kit-8 (CCK-8) assay. Comet and fast halo assays were used to quantify single-strand DNA breaks in TM4 cells. To detect changes in cell morphology during apoptosis, nuclear staining with Hoechst 33342 was performed. An immunofluorescence assay was employed to examine the expression level of proteins connexin 43 and Claudin 11 in TM4 cells after exposure to PNNP concentration of 125 µg/mL. Results: The synthesized PNNP had a size of 170.6 nm, a polydispersity index of 0.269, a zeta potential of +37.8 mV, and a good entrapment efficiency of 71.0%. Encapsulation of Phyllanthus niruri into ChNP induced DNA damage in TM4 cells as determined by alkaline comet and fast halo assay (FHA). Additionally, it stimulated apoptosis, as determined by changes in cell morphology by Hoechst 33342 staining. There was significant down regulation of blood-testis barrier (BTB) proteins in TM4 cells after exposure to PNNP which could compromise the integrity of BTB and subsequently disrupt spermatogenesis process in male. Conclusion: Our investigation confirms the cytotoxic and genotoxic effects of PNNP in TM4 cells, which could lead to spermatogenesis disruption and male infertility.

Formulation of Letrozole-loaded Ethyl Cellulose and Eudragit S100 Nanoparticles by Nanoprecipitation Technique and Determination of Cytotoxic Activity by MTT Assay

Introduction:: The major goal of this work is to develop letrozole nanoparticles using the polymer precipitation technique. Formulations were prepared by using Ethyl cellulose and Eudragit S100 as polymers. Methods:: By varying drug-polymer ratios, a total of ten formulations were prepared. By altering the drug concentration to polymer, five formulations were prepared with Ethyl cellulose and five with Eudragit S100. All ten formulations were evaluated for different characterization and evaluation parameters such as Entrapment efficiency, Loading capacity and in vitro drug release studies, particle size, stability (zeta potential), surface morphology, and drug-polymer interaction study. Result:: In comparison, the NEC 2:1 formulation showed the smallest particle size,high stability, good entrapment efficiency, and sustained drug release. This formulation was further studied to determine the anticancer activity in vitro in the MCF-7 Breast cancer cell line by MTT assay. The results indicated that the prepared formulation exhibited anticancer activity with an IC50 value of 91.26 micromolar. Conclusion:: Comparatively, Ethyl cellulose was proven to be a better polymer than Eudragit S100, and the nanoprecipitation technique was considered the most suitable technique for preparing letrozole nanoparticles.

18-β-Glycyrrhetinic acid encapsulated PLGA nanoparticles attenuate lung cancer proliferation and migration

Conventional treatment methods to treat lung cancer include radiation therapy, chemotherapy, and immunotherapy. However, they cause severe adverse effects and recurrence risk. 18-β-glycyrrhetinic acid (18-β-Gly), a naturally occurring bioactive compound extracted from the liquorice plant has demonstrated anticancer potential by suppressing cancer cell growth, angiogenesis, and metastasis. Although 18-β-Gly possesses potential therapeutic abilities, the application of 18-β-Gly into clinical practices is hindered due to its inferior physicochemical characteristics such as poor bioavailability and low water solubility. Poly lactic-co-glycolic acid (PLGA) is a synthetic polymer with great tuneable options for a nano-drug delivery system used for various diseases, including cancer. Formulating 18-β-Gly into PLGA has helped to overcome challenges imposed by the poor physicochemical characteristics of 18-β-Gly. For this research, 18-β-Gly-PLGA was tested for its anticancer ability using A549 human lung adenocarcinoma lines found in lung cancer. Findings showed that 18-β-Gly-PLGA has favourable physicochemical characteristics, such as sustained in vitro drug release and good entrapment efficiency. 18-β-Gly-PLGA was also able to inhibit 15% and 50% proliferation of A549 cells at 2.5 μM and 50 μM respectively and 28% inhibition of A549 cell migration at 5 μM concentration. Oncogenes such as KRT18, EGFR, BRAF and KRAS were significantly downregulated by 43%, 19.3%, 14.7% and 13.7% respectively as part of the anticancer effects and the underlying mechanism of 18-β-Gly-PLGA. Significant reduction in the expression of cancer proliferation and migration-associated proteins such as receptor tyrosine-protein kinase ErbB2, survivin, macrophage colony-stimulating factor and mesothelin was also observed. The findings of this study demonstrate the promising potential of 18-β-Gly-PLGA as a potential anticancer agent.

Quality by Design Enabled Formulation Optimization of Rabeprazole Sodium Mucoadhesive Microcapsules for the Treatment of Gastroesophageal Reflux Disease

Aims: The present research describes the implementation of quality by-design principles for developing the mucoadhesive microcapsules of rabeprazole sodium for treating gastroesophageal reflux disease conditions. Background: In addition, a holistic QbD-based product development strategy was implemented, where the target product profile was defined based on desired product quality of mucoadhesive microcapsules. Based on TPP, the critical quality attributes were identified. The identification of CMAs was carried out with the help of risk assessment and factor screening exercises, which indicated drugpolymer ratio (X1), temperature (X2), and stirring speed (X3) as the influential factors. Methods: The mucoadhesive microcapsules of rabeprazole sodium were prepared by a solvent evaporation method, and 33 Box-Behnken optimization design was used for the optimization of the selected factors, and mucoadhesive microcapsules formulations were evaluated for particle size (μm), drug entrapment efficiency (%), mucoadhesion (%), and in vitro drug release (Q18h) in percentage characteristics. Mathematical data analysis was performed to fit the two-factor interaction model, and optimized mucoadhesive microcapsules formulation was selected. Results: The optimized mucoadhesive microcapsules indicated desired formulation characteristics with smaller particle size, good entrapment efficiency, better mucoadhesion, and sustained drug release characteristics. Conclusion: In a nutshell, the studies vouch for the successful development of mucoadhesive microcapsules for oral delivery of rabeprazole sodium which could be used to manage gastroesophageal reflux disease condition.

Development and characterization of niosomes loaded mucoadhesive biodegradable ocular inserts for extended release of pilocarpine HCl

Abstract Background Pilocarpine HCl is a non-selective muscarinic receptor agonist that is prescribed for the treatment of glaucoma. The use of pilocarpine conventional eye drops is associated with several side effects, such as loss of visual acuity, and the need for several applications due to rapid drainage away via the nasolacrimal duct, especially for elderly people. Such adverse effects can lead to low patient compliance and poor clinical outcomes. Therefore, the aim of this project was to develop, optimise and characterise a biodegradable pilocarpine HCl ocular insert using niosomes as a drug delivery vehicle. To achieve that, various polymers such as hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), and a blend of both were investigated to prepare the ocular inserts using solvent casting technique. The niosomes of pilocarpine HCl were prepared using span-60 and cholesterol by thin film hydration method. The produced noisome-loaded ocular inserts were characterised using various analytical techniques, including Fourier Transform Infrared (FTIR), X-ray Diffractions (XRD), thermal analysis, particle size analysis, weight and content uniformity, surface pH and drug release profile, among others. Results The results indicated that drug-free ocular inserts of the two polymers (HPMC + PVA) were better than single polymer-based ocular inserts (HPMC or PVA alone). The formed niosomes demonstrated good entrapment efficiency of 49.7% ± 7.0, with an average particle size of 325.7 ± 3.5 nm. The FTIR analysis showed no interaction between the compositions of niosomes. Four optimal formulations with various co-polymer ratios and pilocarpine content were further evaluated. Pilocarpine-containing niosomes-loaded ocular inserts provided uniformity in pilocarpine content (89–96%), with 34.8% moisture content and an average pH of 7. The release profile of niosomes-loaded inserts demonstrated an initial burst release within 2 h ranging from 26.54% (T4) to 41.22% (T2), and continuous sustained release for the next 24 h (68.32 ± 5.11% (T4) to 82.11 ± 6.01% (T2)). Conclusions This work successfully optimised biodegradable ocular inserts containing slow-release pilocarpine HCl encapsulated in niosomes for the treatment of glaucoma without dose dumping, resulting in a user-friendly drug delivery system. Graphical abstract

Designing a nanoliposome loaded with provitamin A xanthophyll β-cryptoxanthin from K. marina DAGII to target a population suffering from hypovitaminosis A

β-cryptoxanthin (β-crx) is a provitamin A carotenoid, ideal for targeting Vitamin A deficiency (VAD); however, its instability and uncontrolled release limit its biological properties. β-crx encapsulated soy phosphatidylcholine nanoliposome was designed to target VAD, and it showed good entrapment efficiency (96.11 ± 0.79%) and desirable size (64.34 ± 1.42 nm), zeta-potential (−17.5 ± 1.70 mV) and polydispersity index (0.288 ± 0.004), suggesting a stable and efficient encapsulation. The spherical nanoliposome was characterized through Field emission scanning electron microscope, Fourier Transform Infrared Spectroscopy, and X-ray diffraction analysis. The nanoliposome retained 74.12 ± 2.08% of β-crx at 4 °C after 30 days of storage at pH 7.4. Bioaccessibility study showed the release of β-crx was less in the gastric medium (5.93 ± 0.68%) compared to intestinal digestion (54.63 ± 0.11%), coinciding with the site of vitamin A metabolism. The residual scavenging activity (67.05 ± 1.53%) increased in the intestinal digestion. The DPPH radical scavenging activity was 82.59 ± 0.43% and inhibited 55.73 ± 0.48% protein oxidation. The TBARS value of 0.493 ± 0.02 mg/L was obtained after 30 days of storage, preventing lipid peroxidation. No chromosomal aberration was observed in the genotoxicity study. It prevented the lysis of erythrocytes, confirmed by the haemolytic assay. The study helps in designing a liposome for the delivery of β-crx to generate new fortified food to prevent VAD.

Formulation Development and Evaluation Studies of Linezolid Inhaler in the Treatment of Tuberculosis

The primary objective of this study was to prepare and evaluate a linezolid inhaler. Dry powder inhaler liposomes were formulated to investigate the efficacy of pulmonary delivery of linezolid for tuberculosis. The liposomes were prepared using soya lecithin and cholesterol in different weight ratios, constant amounts of drugs, and two methods: physical dispersion and ethanol injection. The F9 formulation was characterized for physical and chemical properties such as vesicle size, shape, and zeta potential. The results of physical characterization, in-vitro testing, and stability studies indicate that liposomes containing linezolid can be used for the treatment of tuberculosis. The evaluated batch exhibited favorable physicochemical properties, with spherical liposomes having a mean size below 100 nm and high entrapment efficiency (98.8%). The prepared liposomal dry powder inhalers (DPIs) sustained drug release for up to 8 hours. Liposome stability was assessed 90 days after storage at room temperature, revealing its stability. The liposomal formulation had steady zeta potential, good entrapment efficiency, improved stability, and an extended drug release time. In conclusion, linezolid-loaded liposomal inhalers were successfully formulated.

Formulation and evaluation of thiabendazole-loaded nanoparticles

Therefore, there is a need to develop alternative novel drug delivery formulations of Thiabendazole to improve its intestinal absorption and reduce its side effects during regular therapy. The Thiabendazole nanoparticles were prepared by hot homogenization method under high magnetic stirring using stearic acid as lipid, and poloxamer 188 was used as a surfactant. Initial pre-formulation studies using FTIR spectroscopy reveal that there are no interactions between Thiabendazole and other excipients; hence, they can be used to prepare nanoparticles. The entrapment efficiencies varied from a minimum of 43.62±0.93 to a maximum of 82.14 ± 0.61%, and it can be concluded that a higher amount of lipid is necessary for obtaining a good entrapment efficiency. The drug content of Thiabendazole nanoparticles for all formulations ranges from 66.8 % to 99.3%. A spherical shape was observed for the particles, and the particles had a smooth morphology when examined under SEM. In vitro release studies of the formulations carried out in pH 7.4 PBS showed that the total amount of drug is released for 9 hours with sustained effect. The formulations showed a drastic increase in size when stored at room temperature, where particles increased from an initial to 345.9 ±8.9 nm at the end of 1 month to 899.7 ± 5.8 nm at the end of 2 months. The entrapment efficiency of the formulation was determined at each interval to ensure that the drug molecules didn't undergo any degradation during storage.

Formulation and evaluation of triclabendazole nanoparticles

The aim of the study is the formulation and evaluation of triclabendazole nanoparticles. There is a need to develop alternative novel drug delivery formulations of Triclabendazole to improve its intestinal absorption and also reduce its side effects during regular therapy. The Triclabendazole nanoparticles were prepared by hot homogenization method under high magnetic stirring using stearic acid as lipid, and poloxamer 188 was used as a surfactant. Initial pre-formulation studies using FTIR spectroscopy reveal no interactions between Triclabendazole and other excipients; hence, they can be used for the preparation of nanoparticles. The entrapment efficiencies varied from a minimum of 44.63 ± 0.94 to 83.15 ± 0.62%, and it can be concluded that higher amount of lipid is necessary for obtaining a good entrapment efficiency. The drug content of Triclabendazolenanoparticles for all formulations ranges from 65.9 % to 98.4%. Triclabendazole, being a hydrophobic drug, has moderate entrapment efficiency. A spherical shape was observed for the particles, and the particles had a smooth morphology when examined under SEM. In vitro release studies of the formulations carried out in pH 7.4 PBS showed that the total amount of drug is released for 9hrs with sustained effect. The formulations showed a drastic increase in size when stored at room temperature, where particles increased from an initial to 346.8 ±8.8 nm at the end of 1 month to 899.8 ± 5.9 nm at the end of 2 months. The entrapment efficiency of the formulation was determined at each interval to ensure that the drug molecules didn't undergo any degradation during storage.

Propolis-Based Nanostructured Lipid Carriers for α-Mangostin Delivery: Formulation, Characterization, and In Vitro Antioxidant Activity Evaluation.

α-Mangostin (a xanthone derivative found in the pericarp of Garcinia mangostana L.) and propolis extract (which is rich in flavonoids and phenols) are known for their antioxidant properties, making them potential supplements for the treatment of oxidative stress-related conditions. However, these two potential substances have the same primary drawback, which is low solubility in water. The low water solubility of α-mangostin and propolis can be overcome by utilizing nanotechnology approaches. In this study, a propolis-based nanostructured lipid carrier (NLC) system was formulated to enhance the delivery of α-mangostin. The aim of this study was to characterize the formulation and investigate its influence on the antioxidant activity of α-mangostin. The results showed that both unloaded propolis-based NLC (NLC-P) and α-mangostin-loaded propolis-based NLC (NLC-P-α-M) had nanoscale particle sizes (72.7 ± 1.082 nm and 80.3 ± 1.015 nm, respectively), neutral surface zeta potential (ranging between +10 mV and -10 mV), and good particle size distribution (indicated by a polydispersity index of <0.3). The NLC-P-α-M exhibited good entrapment efficiency of 87.972 ± 0.246%. Dissolution testing indicated a ~13-fold increase in the solubility of α-mangostin compared to α-mangostin powder alone. The incorporation into the propolis-based NLC system correlated well with the enhanced antioxidant activity of α-mangostin (p < 0.01) compared to NLC-P and α-mangostin alone. Therefore, the modification of the delivery system by incorporating α-mangostin into the propolis-based NLC overcomes the physicochemical challenges of α-mangostin while enhancing its antioxidant effectiveness.

Lysozyme-loaded nanocages in a surgical glue for post-operative wound treatment

The objective of research study was development of cutting-edge nanoarchitectonic-based nanocage glue for effective wound management. Lysozyme-loaded nanocage glue (NRS) were synthesized, optimized, characterized, and evaluated for drug entrapment efficiency, morphological properties, stability, in-vitro and ex-vivo drug release kinetics, transdermal penetration, and animal wound healing efficacy (in-vivo). The lysozyme-loaded nanocages exhibited desirable characteristics, including ultra-small size (240.1 ± 26.73 nm), higher zeta potential (+17.2 ± 0.24 mV), good entrapment efficiency (90.22 ± 1.67%), spherical hollow shape, and spectral shifts resulting in good entrapment. The lysozyme-loaded nanocages displayed a controlled drug release profile and demonstrated a higher wound healing efficacy, with 87% wound closure rate observed by the 9th day. Results showed that adhesives property resulted in high drug contact time giving fast healing in comparison to the control and other treatments with significant impact on wound healing. In conclusion, the development of the nanocage glue observed to be an effective wound adhesive highlighting its significance for clinical wound healing management. The results suggest that the nanoarchitectonic-based nanocage glue potential candidature for wound healing applications and improved treatments with better outcomes for patients.

Combinatorial drug-loaded quality by design adapted transliposome gel formulation for dermal delivery: In vitro and dermatokinetic study.

Ursolic acid is a powerful drug that possesses many therapeutic properties, such as hepatoprotection, immunomodulation, anti-inflammatory, antidiabetic, antibacterial, antiviral, antiulcer, and anticancer activity. Centella asiatica (L.) Urban (Umbelliferae) contains a triterpene called asiatic acid, which has been used effectively in traditional Chinese and Indian medicine system for centuries. Anticancer, anti-inflammatory, and neuroprotective properties are only some of the many pharmacological actions previously attributed to asiatic acid . The present work developed an optimized combinatorial drug-loaded nano-formulation by Quality by design approach. The optimize transliposome for accentuated dermal delivery of dual drug. The optimization of drug-loaded transliposome was done using the "Box-Behnken design." The optimized formulation was characterized for vesicles size, entrapment efficiency (%), and in vitro drug release. Additionally, transmission electron microscopy (TEM), confocal laser scanning microscopy (CLSM), and dermatokinetic study were performed for further evaluation of drug-loaded optimized transliposome formulation. The optimized combinatorial drug-loaded transliposome formulation showed a particle size of 86.36 ± 2.54 nm, polydispersity index (PDI) 0.230 ± 0.008, and an entrapment efficiency of 87.43 ± 2.66% which depicted good entrapment efficiency. In vitro drug release of ursolic acid and asiatic acid transliposomes was found to be 85.12 ± 2.54% and 80.23 ± 3.23%, respectively, as compared to optimized ursolic acid and asiatic acid transliposome gel drug release that was 67.18 ± 2.85% and 60.28 ± 4.12%, respectively. The skin permeation study of ursolic and asiatic acid conventional formulation was only 32.48 ± 2.42%, compared with optimized combinatorial drug-loaded transliposome gel (79.83 ± 4.52%) at 12 h. After applying combinatorial drug-loaded transliposome gel, rhodamine was able to more easily cross rat skin, as observed by confocal laser scanning microscopy, in comparison with when the rhodamine control solution was used. The UA_AA-TL gel formulation absorbed more ursolic acid and asiatic acid than the UA_AA-CF gel formulation, as per dermatokinetic study. Even after being incorporated into transliposome vesicles, the antioxidant effects of ursolic and asiatic acid were still detectable. In most cases, transliposomes vesicular systems generate depots in the skin's deeper layers and gradually release the medicine over time, allowing for fewer applications. In overall our studies, it may be concluded that developed dual drug-loaded transliposomal formulation has great potential for effective topical drug delivery for skin cancer.

Design and Characterization of an Ethosomal Gel Encapsulating Rosehip Extract

Rising environmental awareness drives green consumers to purchase sustainable cosmetics based on natural bioactive compounds. The aim of this study was to deliver Rosa canina L. extract as a botanical ingredient in an anti-aging gel using an eco-friendly approach. Rosehip extract was first characterized in terms of its antioxidant activity through a DPPH assay and ROS reduction test and then encapsulated in ethosomal vesicles with different percentages of ethanol. All formulations were characterized in terms of size, polydispersity, zeta potential, and entrapment efficiency. Release and skin penetration/permeation data were obtained through in vitro studies, and cell viability was assessed using an MTT assay on WS1 fibroblasts. Finally, ethosomes were incorporated in hyaluronic gels (1% or 2% w/v) to facilitate skin application, and rheological properties were studied. Rosehip extract (1 mg/mL) revealed a high antioxidant activity and was successfully encapsulated in ethosomes containing 30% ethanol, having small sizes (225.4 ± 7.0 nm), low polydispersity (0.26 ± 0.02), and good entrapment efficiency (93.41 ± 5.30%). This formulation incorporated in a hyaluronic gel 1% w/v showed an optimal pH for skin application (5.6 ± 0.2), good spreadability, and stability over 60 days at 4 °C. Considering sustainable ingredients and eco-friendly manufacturing technology, the ethosomal gel of rosehip extract could be an innovative and green anti-aging skincare product.